发明名称 SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
摘要 Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
申请公布号 US2015329497(A1) 申请公布日期 2015.11.19
申请号 US201314652705 申请日期 2013.12.19
申请人 SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE ;DUKE UNIVERSITY 发明人 PINKERTON Anthony;MALONEY Patrick;HERSHBERGER Paul;PEDDIBHOTLA Satyamaheshwar;HEDRICK Michael;BARAK Lawrence;CARON Marc
分类号 C07D239/94;C07D401/04;A61K31/519;C07D403/04;A61K31/5377;C07D471/04;A61K31/517;C07D405/04 主分类号 C07D239/94
代理机构 代理人
主权项 1. A compound of Formula I, or a pharmaceutically acceptable salt, solvate, tautomer, or N-oxide thereof: wherein: A is A1, —O-A1, —NH-A1, —C(═O)-A1, or —S(═O)2-A1; A1 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted 5-membered heteroaryl, optionally substituted 6-membered heteroaryl, optionally substituted 9-membered heteroaryl and optionally substituted 10-membered heteroaryl; wherein optional substituents for A are selected from the group consisting of hydrogen, halogen, —CN, —OH, —NO2, —N(R13)—R14, —C(═O)—N(R13)—R14, —NR13C(═O)R15, —C(═O)—O—R13, —O—C(═O)—R15, —SR13, —S(═O)R15, —S(═O)2R15, —N(R13)S(═O)2R15, —S(═O)2—N(R13)—R14, —C(═O)R13, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted alkoxy, optionally substituted haloalkyl, optionally substituted haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl;B is selected from the group consisting of optionally substituted phenyl, optionally substituted 5-membered heteroaryl, optionally substituted 6-membered heteroaryl, optionally substituted alkyl, optionally substituted cycloalkyl and optionally substituted heterocyloalkyl.Y is selected from optionally substituted heterocyloalkyl, optionally substituted spiroheterocyloalkyl, optionally substituted with alkyl, and —NR2(CH2)nNR3—; n is 2, 3, 4, 5, or 6;R2 is H or alkyl;R3 is H or alkyl;X1 is N or C(R1);X2 is N or C(R1);X3 is N or C(R4);X4 is N or C(R5);X5 is N or C(R6);X6 is N or C(R7);each R1 is independently selected from the group consisting of hydrogen, halogen, —CN, —OH, —NO2, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted haloalkyl, and optionally substituted haloalkoxy;each of R4, R5, R6, and R7 is independently selected from the group consisting of hydrogen, halogen, —CN, —OH, —NO2, —N(R13)—R14, —C(═O)—N(R13)—R14, —NR13C(═O)R15, —C(═O)—O—R13, —O—C(═O)—R15, —SR13, —S(═O)R15, —S(═O)2R15, —N(R13)S(═O)2R15, —S(═O)2—N(R13)—R14, —C(═O)R13, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted alkoxy, optionally substituted haloalkyl, optionally substituted haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl;or R5 and R6 are taken together with the atoms connecting R5 and R6 to form an optionally substituted heterocycloalkyl;each of R13 and R14 is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted alkoxy, optionally substituted haloalkyl, optionally substituted haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl;or R13 and R14, when on the same nitrogen atom, are taken together with the nitrogen atom to which they are attached to form an optionally substituted heterocycloalkyl;R15 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted alkoxy, optionally substituted haloalkyl, optionally substituted haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl.
地址 La Jolla CA US